RU2014115188A - COMBINATION OF PHOSPHATIDYLINOSITOL-3-KINASE (PI3K) INHIBITOR AND mTOR INHIBITOR - Google Patents

COMBINATION OF PHOSPHATIDYLINOSITOL-3-KINASE (PI3K) INHIBITOR AND mTOR INHIBITOR Download PDF

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RU2014115188A
RU2014115188A RU2014115188/15A RU2014115188A RU2014115188A RU 2014115188 A RU2014115188 A RU 2014115188A RU 2014115188/15 A RU2014115188/15 A RU 2014115188/15A RU 2014115188 A RU2014115188 A RU 2014115188A RU 2014115188 A RU2014115188 A RU 2014115188A
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cancer
disease
malignant neoplasm
stomach
prostate
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Карлос ГАРСИЯ-ЭВЕВЕРРИЯ
Сове-Мишель МАИРА
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Новартис Аг
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Abstract

1. Применение соединения, представляющего собой 5-(2,6-диморфолин-4-илпиримидин-4-ил)-4-трифторметилпиридин-2-иламин, или его стереоизомера, таутомера или фармацевтически приемлемой соли для лечения заболевания, представляющего собой рак или злокачественное новообразование, которое зависит от приобретенного фосфорилирования и активации протеинкиназы АКТ в ходе лечения ингибитором mTOR, представляющим собой эверолимус.2. Применение по п. 1, где заболевание, представляющее собой рак или злокачественное новообразование, выбрано из рака молочной железы, почечно-клеточной карциномы, опухолей желудка, нейроэндокринных опухолей, лимфомы и рака предстательной железы.3. Применение по п. 1, где заболевание, которое представляет собой рак или злокачественное новообразование, выбрано из доброкачественной или злокачественной опухоли, рака мозга, почек, печени, надпочечников, мочевого пузыря, молочной железы, желудка, опухолей желудка, яичников, ободочной кишки, прямой кишки, предстательной железы, поджелудочной железы, легких, влагалища или щитовидной железы, саркомы, глиобластомы, множественной миеломы, рака желудочно-кишечного тракта, опухоли шеи и головы, эпидермальной гиперпролиферации, псориаза, гиперплазии предстательной железы, неоплазии эпителиального характера, лимфомы, карциномы молочной железы или лейкоза.4. Применение соединения, представляющего собой 5-(2,6-диморфолин-4-илпиримидин-4-ил)-4-трифторметилпиридин-2-иламин, или его стереоизомер, таутомер или фармацевтически приемлемую соль, для лечения заболевания, представляющего собой рак или злокачественное новообразование, которое приобрело устойчивость или име1. The use of a compound representing 5- (2,6-dimorpholin-4-yl-pyrimidin-4-yl) -4-trifluoromethyl-pyridin-2-ylamine, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for the treatment of a disease, which is cancer or malignant neoplasm, which depends on the acquired phosphorylation and activation of AKT protein kinase during treatment with the mTOR inhibitor, which is everolimus. 2. The use according to claim 1, wherein the disease, which is a cancer or malignant neoplasm, is selected from breast cancer, renal cell carcinoma, tumors of the stomach, neuroendocrine tumors, lymphoma and prostate cancer. The use according to claim 1, wherein the disease, which is a cancer or malignant neoplasm, is selected from a benign or malignant tumor, cancer of the brain, kidney, liver, adrenal gland, bladder, breast, stomach, tumors of the stomach, ovaries, colon, rectum bowel, prostate, pancreas, lung, vagina or thyroid gland, sarcoma, glioblastoma, multiple myeloma, cancer of the gastrointestinal tract, neck and head tumor, epidermal hyperproliferation, psoriasis, hyperplasia asia of the prostate gland, epithelial neoplasia, lymphoma, breast carcinoma or leukemia. 4. The use of a compound representing 5- (2,6-dimorpholin-4-yl-pyrimidin-4-yl) -4-trifluoromethyl-pyridin-2-ylamine, or its stereoisomer, tautomer or pharmaceutically acceptable salt, for the treatment of a disease representing cancer or malignant neoplasm that has become resistant or has

Claims (4)

1. Применение соединения, представляющего собой 5-(2,6-диморфолин-4-илпиримидин-4-ил)-4-трифторметилпиридин-2-иламин, или его стереоизомера, таутомера или фармацевтически приемлемой соли для лечения заболевания, представляющего собой рак или злокачественное новообразование, которое зависит от приобретенного фосфорилирования и активации протеинкиназы АКТ в ходе лечения ингибитором mTOR, представляющим собой эверолимус.1. The use of a compound representing 5- (2,6-dimorpholin-4-yl-pyrimidin-4-yl) -4-trifluoromethyl-pyridin-2-ylamine, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for the treatment of a disease, which is cancer or malignant neoplasm, which depends on the acquired phosphorylation and activation of AKT protein kinase during treatment with the mTOR inhibitor, which is everolimus. 2. Применение по п. 1, где заболевание, представляющее собой рак или злокачественное новообразование, выбрано из рака молочной железы, почечно-клеточной карциномы, опухолей желудка, нейроэндокринных опухолей, лимфомы и рака предстательной железы.2. The use according to claim 1, wherein the disease, which is a cancer or malignant neoplasm, is selected from breast cancer, renal cell carcinoma, tumors of the stomach, neuroendocrine tumors, lymphoma and prostate cancer. 3. Применение по п. 1, где заболевание, которое представляет собой рак или злокачественное новообразование, выбрано из доброкачественной или злокачественной опухоли, рака мозга, почек, печени, надпочечников, мочевого пузыря, молочной железы, желудка, опухолей желудка, яичников, ободочной кишки, прямой кишки, предстательной железы, поджелудочной железы, легких, влагалища или щитовидной железы, саркомы, глиобластомы, множественной миеломы, рака желудочно-кишечного тракта, опухоли шеи и головы, эпидермальной гиперпролиферации, псориаза, гиперплазии предстательной железы, неоплазии эпителиального характера, лимфомы, карциномы молочной железы или лейкоза.3. The use according to claim 1, where the disease, which is a cancer or malignant neoplasm, is selected from a benign or malignant tumor, cancer of the brain, kidney, liver, adrenal gland, bladder, breast, stomach, tumors of the stomach, ovaries, colon , rectum, prostate, pancreas, lung, vagina or thyroid gland, sarcoma, glioblastoma, multiple myeloma, cancer of the gastrointestinal tract, neck and head tumor, epidermal hyperproliferation, psoriasis, hyper lazii prostate neoplasia of epithelial character, lymphomas, breast carcinoma or leukemia. 4. Применение соединения, представляющего собой 5-(2,6-диморфолин-4-илпиримидин-4-ил)-4-трифторметилпиридин-2-иламин, или его стереоизомер, таутомер или фармацевтически приемлемую соль, для лечения заболевания, представляющего собой рак или злокачественное новообразование, которое приобрело устойчивость или имеет пониженную чувствительность к лечению ингибитором mTOR, выбранному из сиролимуса, эверолимуса, CCI-779, ABT578, SAR543, аскомицина, AP23573, AP23841 или KU-0063794. 4. The use of a compound representing 5- (2,6-dimorpholin-4-yl-pyrimidin-4-yl) -4-trifluoromethyl-pyridin-2-ylamine, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for treating a cancer disease or a malignant neoplasm that has acquired resistance or has decreased sensitivity to treatment with an mTOR inhibitor selected from sirolimus, everolimus, CCI-779, ABT578, SAR543, ascomycin, AP23573, AP23841 or KU-0063794.
RU2014115188/15A 2008-10-31 2014-04-15 COMBINATION OF PHOSPHATIDYLINOSITOL-3-KINASE (PI3K) INHIBITOR AND mTOR INHIBITOR RU2014115188A (en)

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